Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential...

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Main Authors: Brem, J, Panduwawala, T, Hansen, JU, Hewitt, J, Liepins, E, Donets, P, Espina, L, Farley, AJM, Shubin, K, Campillos, GG, Kiuru, P, Shishodia, S, Krahn, D, Leśniak, RK, Schmidt Adrian, J, Calvopiña, K, Turrientes, M-C, Kavanagh, ME, Lubriks, D, Hinchliffe, P, Langley, GW, Aboklaish, AF, Eneroth, A, Backlund, M, Baran, AG, Nielsen, EI, Speake, M, Kuka, J, Robinson, J, Grinberga, S, Robinson, L, McDonough, MA, Rydzik, AM, Leissing, TM, Jimenez-Castellanos, JC, Avison, MB, Da Silva Pinto, S, Pannifer, AD, Martjuga, M, Widlake, E, Priede, M, Hopkins Navratilova, I, Gniadkowski, M, Belfrage, AK, Brandt, P, Yli-Kauhaluoma, J, Bacque, E, Page, MGP, Björkling, F, Tyrrell, JM, Spencer, J, Lang, PA, Baranczewski, P, Cantón, R, McElroy, SP, Jones, PS, Baquero, F, Suna , E, Morrison, A, Walsh, TR, Schofield, CJ
Format: Journal article
Language:English
Published: Springer Nature 2021

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